Receptor Interacting Protein Kinase 1 (RIP1) has been implicated as a key contributor to inflammation through the regulation of programmed necrosis. Inhibition of this kinase has been shown to hinder cell necrotic death, thereby establishing RIP1 as a viable target for the potential treatment of multiple inflammatory diseases. A novel benzoxazepinone (BOAz) series of RIP1 inhibitors, represented by GSK481, was discovered from a focused screen using a three-cycle amino acid core DNA-encoded library. BOAz has demonstrated outstanding <i>in vitro</i> potencies, excellent developability properties, and extraordinary cross-kinase selectivity.

Get “RIP”ped: Discovery of a lean & mean atypical kinase scaffold for the selective inhibition of RIP1

251st National Meeting (2016)

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